Delving into the Latest Updates on Eupatilin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Eupatilin/jaceosidin, Jaceosidin/eupatilin, Stillen

+ [2]

Target-

Mechanism-

Therapeutic Areas

Digestive System DisordersImmune System Diseases

Active Indication

GastritisStomach UlcerAnaphylaxis

Inactive Indication-

Originator Organization

Dong-A Pharmaceutical Co., Ltd.

Active Organization

Dong-A Pharmaceutical Co., Ltd.

Sungkyunkwan UniversitySamsung Biomedical Research Institute

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

KR (29 Apr 2005),

GastritisStomach Ulcer

Regulation-

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Structure

Molecular FormulaC18H16O7

InChIKeyDRRWBCNQOKKKOL-UHFFFAOYSA-N

CAS Registry22368-21-4

Jaceosidin (JAC) is a natural flavonoid with anti-oxidant and other pharmacological activities; however, its anti-cancer mechanism remains unclear. We investigated the mechanism of action of JAC in gastric cancer cells. Cytotoxicity and apoptosis assays showed that JAC effectively killed multiple gastric cancer cells and induced apoptosis in human gastric adenocarcinoma AGS cells via the mitochondrial pathway. Network pharmacological analysis suggested that its activity was linked to reactive oxygen species (ROS), AKT, and MAPK signaling pathways. Furthermore, JAC accumulated ROS to up-regulate p-JNK, p-p38, and IκB-α protein expressions and down-regulate the p-ERK, p-STAT3, and NF-κB protein expressions. Cell cycle assay results showed that JAC accumulated ROS to up-regulate p21 and p27 protein expressions and down-regulate p-AKT, CDK2, CDK4, CDK6, Cyclin D1, and Cyclin E protein expressions to induce G0/G1 phase arrest. Cell migration assay results showed JAC accumulated ROS to down-regulate Wnt-3a, p-GSK-3β, N-cadherin, and β-catenin protein expressions and up-regulate E-cadherin protein expression to inhibit migration. Furthermore, N-acetyl cysteine pre-treatment prevented the change of these protein expressions. In summary, JAC induced apoptosis and G0/G1 phase arrest and inhibited migration through ROS-mediated signaling pathways in AGS cells.

05 Nov 2024·Anti-Cancer Agents in Medicinal Chemistry

Composition and Biological Activity of Flavonoid-containing Fractions of an Extract from Gratiola officinalis L.

Article

Author: Polukonova, Anna ; Mudrak, Dmitry ; Mylnikov, Artyom ; Bucharskaya, Alla ; Matora, Larisa ; Shirokov, Alexander ; Polukonova, Natalya ; Fedonenko, Yulia ; Kanevskiy, Matvey ; Grinev, Vyacheslav ; Navolokin, Nikita ; Maslyakova, Galina

Introduction:Gratiola officinalis L. (hedge hyssop), a medicinal plant of the Scrophulariaceae family, has diuretic, purgative, and vermifuge properties. It is used as a herbal tea to treat chronic gastroenteritis, renal colic, jaundice, and intestinal worms. Previously, we have found that an extract from G. officinalis is nontoxic and has antitumor, antioxidant, antimicrobial, antiinflammatory, anticachexic, and other properties. Our aims in this study were to separate the G. officinalis extract into individual fractions, to identify the most biologically active fractions, and to examine the chemical composition of these fractions and their biological activity toward A498 renal carcinoma cells.Methods:The G. officinalis extract was fractionated by reversed-phase high-performance liquid chromatography, and each fraction was tested for antitumor activity. The active fractions were characterized by UV–visible electron spectral analysis, circular dichroism analysis, Fourier transform infrared spectroscopy, high-performance liquid chromatography, electrospray ionization tandem mass spectrometry, and nuclear magnetic resonance spectroscopy.Results:Two antitumor-active fractions of a flavonoid nature were isolated and chromatographically purified. On the basis of the nuclear magnetic resonance data, the aglycone fragment of the main component of one fraction was found to be structured as 2-(3,4-dimethoxyphenyl)-7-hydroxychroman-4-one, or 3',4'-dimethoxy-7- hydroxyflavanone.Conclusion:The antitumor effect of the most active fraction containing 7-O-glucoside of apigenin, glycoside 7,3'-di-O-luteolin and trace amounts of eupatilin against renal carcinoma A498 cells was manifested in its cytotoxic, cytostatic, apoptotic and autophagosomal activities. In addition, we found 3-(1-2)-glucoside of soyaspogenol B, which is a pentacyclic triterpenoid in the structure.

18 Oct 2024·Medicina (Kaunas, Lithuania)

The Effect of CKD-495, Eupacidin, and Their Marker Compounds on Altered Permeability in a Postoperative Ileus Animal Model.

Article

Author: Lee, Young Ju ; Kim, Min-Jae ; Park, Hyojin ; Hussain, Zahid

Background and Objectives: Postoperative ileus (POI) is a delay in gastrointestinal transit following surgery that leads to various complications. There is limited understanding of its effective treatment options. CKD-495 and eupacidin are natural products licensed for treating mucosal lesions in acute and chronic gastritis; however, little is known about their effects on intestinal permeability. This study evaluated the effects of CKD-495, eupacidin, and its components (eupatilin and cinnamic acid) on intestinal permeability in an animal model of POI. Materials and Methods: Guinea pigs underwent surgical procedures and were randomly assigned to different treatment groups. Drugs were administered orally prior to surgery. Intestinal permeability, leukocyte count, and the expression of calprotectin and tight junction proteins were measured in the harvested ileum tissue. Results: The intestinal permeability and leukocyte count were higher in the POI group than in the control group. The pre-administration of CKD-495, cinnamic acid, eupacidin, and eupatilin effectively prevented these changes in the POI model. No significant differences were observed in the expression of tight junction proteins. Conclusions: CKD-495, cinnamic acid, eupacidin, and eupatilin exerted protective effects against increased intestinal permeability and inflammation in an animal model of POI. These natural products have potential as therapeutic options for the treatment of POI.

100 Deals associated with Eupatilin

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	A02B	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Gastritis	KR	Dong-A Pharmaceutical Co., Ltd.	29 Apr 2005
Stomach Ulcer	KR	Dong-A Pharmaceutical Co., Ltd.	29 Apr 2005

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Anaphylaxis	Discovery	KR	Sungkyunkwan University	20 Mar 2005
Anaphylaxis	Discovery	KR	Samsung Biomedical Research Institute	20 Mar 2005

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


UEGW2022	Not Applicable	-	-	Eupatilin	kxqlmgmvxu(akvcrwzeuk) = njhvjkxbwx huxhxipzbs (rcobjuqsxy )	-	09 Oct 2022
				Aspirin	kxqlmgmvxu(akvcrwzeuk) = jiohxdvhlu huxhxipzbs (rcobjuqsxy )
NCT02282670 (Pubmed)	Phase 3	Gastritis	434	DA-5204	(gfywheiotr) = AEs were reported in 18 (8.4%) patients in the DA-5204 group and 19 (8.8%) in the DA-9601 group xstqcmrhcb (mavcwnazpu )	Positive	01 Nov 2017
				DA-9601